Proton pump

Bafilomycin A1 belongs to the macrolide class of antibiotics and is a V-ATPase inhibitor (IC50=0.44 nM) that is specific and reversible. Bafilomycin A1 is an inhibitor of the late phase of autophagy, blocking the fusion of autophagosomes with lysosomes. Bafilomycin A1 also induces apoptosis.

Chebulinic acid is a potent inhibitor of M. tuberculosis DNA gyrase. It also can inhibit SMAD-3 phosphorylation and H+ K+-ATPase activity.

Pumaprazole (BY-841) is an antagonist of a reversible proton pump.

Saviprazole (Hoe-731), a proton pump inhibitor, is used potentially for treatment of gastric ulcer.

Abscisic Acid (Dormin) is a plant hormone, which is involved in many plant developmental processes, modulates ion homeostasis and metabolism, and inhibits germination and seedling growth.

EN6-mediated ATP6V1A modification decouples the v-ATPase from the Rags, leading to inhibition of mTORC1 signaling, increased lysosomal acidification and activation of autophagy. EN6 clears TDP-43 aggregates, a causative agent in frontotemporal dementia, in a lysosome-dependent manner. EN6 is a small-molecule in vivo activator of autophagy that covalently targets cysteine 277 in the ATP6V1A subunit of the lysosomal the vacuolar H+ ATPase (v-ATPase).

WY-47766 (OST-766) is a small molecule proton pump inhibitor that can be used to study postmenopausal osteoporosis.

Omeprazole (Losec) is a proton pump inhibitor (PPI), Omeprazole(Losec) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).

Zinc pyrithione (OM-1563), an antibacterial and antifungal agent can disrupt membrane transport by blocking the proton pump.

Caloxin 2A1 acetate is an inhibitor of extracellular plasma membrane Ca2+-ATPase (PMCA) peptide. Caloxin 2A1 acetate inhibits Ca2+-dependent formation of the 140-kDa acid-stable acylphosphate.

Thonzonium bromide is a mono-cationic surfactant that is structurally similar to Farnesol as an antimicrobial agent. It inhibits proton transport in a dose-dependent manner (EC50=69 μM). It inhibits RANKL-induced osteoclast formation and bone resorption in vitro and prevents LPS-induced bone loss in vivo.

Ilaprazole (IY-81149) is a proton pump inhibitor used in the treatment of dyspepsia gastroesophageal reflux disease (GORD GERD) and duodenal ulcer. Studies also showed that Ilaprazole significantly prevented the development of reflux oesophagitis.

SCH28080 is a reversible and K+-competitive inhibitor of gastric H+ K+-ATPase with an IC50 value of 20 nM (rabbit microsomal membrane).SCH28080 is a potent inhibitor of acid secretion in vivo with anti-ulcer activity, anti-secretory and cytoprotective activity.

Lansoprazole (A-65006) is a 2, 2, 2-trifluoroethoxypyridyl derivative of timoprazole that is used in the therapy of STOMACH ULCERS and ZOLLINGER-ELLISON SYNDROME. The drug inhibits H(+)-K(+)-EXCHANGING ATPASE which is found in GASTRIC PARIETAL CELLS. Lansoprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

Rabeprazole sodium (Habeprazole Sodium) is a 4-(3-methoxypropoxy)-3-methylpyridinyl derivative of timoprazole that is used in the therapy of stomach ulcers and Zollinger-Ellison syndrome. The drug inhibits H(+)-K(+)-exchanging ATPase which is found in gastric parietal cells.

5-Hydroxylansoprazole (AG1908) is an active metabolite of Lansoprazole, a gastric proton-pump inhibitor used to treat various peptic diseases. Lansoprazole is metabolized through CYP2C19, resulting in the formation of 5-Hydroxylansoprazole[1][2].

Ilaprazole sodium (IY-81149 sodium) , a substituted benzimidazole prodrug, is a selective and irreversible proton pump inhibitor. A weak base, Ilaprazole accumulates in the acidic environment of the secretory canaliculus of the gastric parietal cell where it is converted to an active sulfenamide form that binds to cysteine sulfhydryl groups on the luminal aspect of the proton pump hydrogen-potassium adenosine triphosphatase (H+ K+ ATPase), thereby inhibiting the pump's activity and the parietal cell secretion of H+ ions into the gastric lumen, the final step in gastric acid production.

(R)-Lansoprazole (T 168390) is the R-isomer of lansoprazole and a substituted benzimidazole prodrug with selective and irreversible proton pump inhibitor activity.Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor)

Pantoprazole (BY1023) is a proton pump inhibitor used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.

Omeprazole sulfone is a metabolite of Omeprazole that inhibits the proton pump.

Diphyllin could be characterized as a new V-ATPase inhibitor in treating gastric cancer and inhibiting the phosphorylation of LRP6 in Wnt β-catenin signaling.

Pantoprazole sodium (Pantecta) is the sodium salt form of a substituted benzimidazole with proton pump inhibitor activity. Pantoprazole sodium is a lipophilic, weak base that crosses the parietal cell membrane and enters the acidic parietal cell canaliculus where it becomes protonated, producing the active metabolite sulfenamide, which forms an irreversible covalent bond with two sites of the H+ K+-ATPase enzyme located on the gastric parietal cell, thereby inhibiting both basal and stimulated gastric acid production.

Esomeprazole Sodium ((S)-Omeprazole sodium) is the S-isomer of omeprazole with selective and irreversible proton pump inhibitor activity.Esomeprazole acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H+-ATPases

Tegoprazan is an orally active, highly selective gastric H+ K+-ATPase inhibitor that controls gastric acid secretion and motility, with an IC50 of 0.29-0.52 μM for porcine, canine, and human H+ K+-ATPase in vitro.

Vonoprazan (TAK-438 (free base)) is an orally active potassium-competitive acid blocker.Vonoprazan can be used for the treatment of gastroduodenal ulcer and reflux esophagitis

Tenatoprazole (TU-199), a prodrug of the proton pump inhibitor (PPI) class, can inhibit proton transport (IC50: 3.2 μM).

Lansoprazole sodium (Lansoprazole (sodium)) is a proton pump inhibitor (PPI) and a potent inhibitor of gastric acidity which is widely used in the therapy of gastroesophageal reflux and peptic ulcer disease.

Ilaprazole (IY-81149) sodium hydrate is an orally active proton pump inhibitor that irreversibly inhibits H+ K+-ATPase in rabbit parietal cells with a dose-dependent IC50 of 6 μM. It is used in gastric ulcer research and acts as a potent inhibitor of T-lymphokine-activated killer cell-originated protein kinase (TOPK) [1] [2].

Pantoprazole Sodium Hydrate (BY1023 (sodium hydrate)) is a proton pump inhibitor drug, used for short-term treatment of erosion and ulceration of the esophagus caused by gastroesophageal reflux disease.

Omeprazole Sodium is a proton pump inhibitor(PPI) and suppresses gastric acid secretion. Omeprazole Sodium is a potent neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor). Omeprazole Sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole Sodium inhibits growth of Gram-positive and Gram-negative bacteria.

Rabeprazole Sulfide (Rabeprazole Related Compound E) is an antiulcer drug in the class of proton pump inhibitors.

Esomeprazole Magnesium trihydrate ((S)-Omeprazole magnesium trihydrate) is a proton pump inhibitor indicated for the short-term treatment of gastroesophageal reflux disease in patients with a history of erosive esophagitis.Esomeprazole magnesium trihydrate acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H+-ATPases

Esomeprazole Magnesium (NEXIUM) is the S-isomer of omeprazole, can reduce gastric acid secretion with selective and irreversible proton pump inhibitor activity.Esomeprazole magnesium acts as an exosome inhibitor by blocking the exosome release via the inhibition of V-H+-ATPases

Esomeprazole is the S-isomer of omeprazole, inhibits the lysosomal cysteine protease legumain to prevent cancer metastasis. Esomeprazole is a proton pump inhibitors (PPI).

Omeprazole sulfide (Ufiprazole), a metabolite of Omeprazole, functions as a proton pump inhibitor.

Vonoprazan Fumarate (TAK438) , a novel potassium-competitive acid blocker, inhibits gastric acid secretion. Vonoprazan Fumarate (TAK438) inhibited H+,K+-ATPase activity in porcine gastric microsomes with IC50 value of 19 nM at pH 6.5.

Abeprazan hydrochloride (Fexuprazan hydrochloride) is an effective reversible potassium-competitive acid blocker with oral activity, inhibiting H+, K+ -atPase by competitive binding to potassium ions without acid activation. Abeprazan hydrochloride is a proton pump inhibitor (PPI) that acts by reducing gastric acid production and is used to treat gastric acid-related disorders, such as gastroesophageal reflux disease (GERD) and peptic ulcers.

Bamaquimast (L 0042) is a proton pump inhibitor for the study of asthma-like immune system disorders and respiratory diseases.

Levolansoprazole ((S)-Lansoprazole), a proton pump inhibitor, irreversibly inhibits H+ K+-stimulated ATPase pumps in parietal cells (IC50: 5.2 μM). It also inhibits acid formation in isolated canine parietal cells (IC50: 82 μM). Both (R)- and (S)-lansoprazole are pharmacologically active with similar potencies.

Verucopeptin is a pyranized cyclic peptide and an inhibitor of hypoxia-inducible factor 1 (HIF-1). It is an antibiotic effective against B16 melanoma, with anticancer activity, lowering the expression of HIF-1 target genes and HIF-1α protein levels. It can be used in cancer research.

S-Pantoprazole (sodium trihydrate), a variant of Pantoprazole, is pivotal in managing diseases associated with gastric acid secretion disorders, serving as a proton pump inhibitor [1].

The compound cis-3-Indoleacrylic acid acts as a nematicidal agent and can be isolated from Streptomyces youssoufiensis YMF3.862. It functions as a V-ATPase inhibitor, reducing both the expression and enzymatic activity of V-ATPase. Additionally, cis-3-Indoleacrylic acid causes swelling in Meloidogyne incognita larvae and notable cracking on the cuticle surface [LC50: 16.31 μg mL]. It also inhibits the accumulation of H+ within nematodes.

V-ATPase-IN-1 (Compound 3b-03) is an inhibitor of Vacuolar-type H+-ATPases (V-ATPase), exhibiting an inhibition constant (IC50) of 194.80 μM and effectively targeting the V-ATPase subunit A with a dissociation constant (Kd) of 0.803 μM. This compound demonstrates insecticidal activity against M. separata (LC50 = 2.64 mM), aiding in the development of chemical insecticides.